Claims for Patent: 4,866,036

Summary for Patent: 4,866,036

Title:	Dipeptidyl 5-0,6-0-acyl-2-amino-2-deoxy-D-glucofuranose compositions and methods of use in aids-immunocompromised human hosts
Abstract:	Disclosed are specific dipeptidyl 5-0, 6-0-Acyl-2-amino-2-deoxy-D-glucofuranoses, which, either alone, or in combination with an anti-AIDS drug, e.g. azidothymidine, provide protection in human individuals whose resistance to infection has been specifically suppressed by an AIDS-related (HIV) virus, as well as help to suppress the AIDS-related infection itself.
Inventor(s):	Durette; Philippe L. (New Providence, NJ)
Assignee:	Merck & Co., Inc. (Rahway, NJ)
Application Number:	07/105,057
Patent Claims:	1. A composition for enhancing host resistance against opportunistic bacterial, fungal or viral infection in a human host immunocompromised by an AIDS-related virus comprising a compound of the formula: ##STR11## wherein: R.sub.1 is C.sub.1-7 alkyl, substituted C.sub.1-7 alkyl; phenyl; or substituted phenyl; R.sub.2 is hydrogen; or C.sub.1-10 alkyl; R.sub.3 and R.sub.4 may be the same independently acyl of the formula: ##STR12## ##STR13## where X is -O-, -S-, or R.sub.9, R.sub.10, and R.sub.12 may be the same or different and are each independently hydrogen; C.sub.1-20 alkyl; C.sub.1-20 alkylcarbonyloxy; amino; benzyl; C.sub.1-20 alkylamido; alkoxymethyl; or C.sub.1-20 alkylamido; r is 0 or 1; s is 0 or 1; and t is 0-20, provided that s may only be 0 when r and t are greater than 0, or when r is 0 and R.sub.11 is amino, phenyl, substituted phenyl, 1-adamantyl, or heterocycle selected from the gorup consisting of 2- or 3-furyl, 2- or 3-thienyl, 2- or 3-pyrrolidinyl, 2-, 3-, or 4-pyridyl, and 1-tetrazolyl, said heterocycle optionally substituted with C.sub.1-20 alkylcarbonyl; and R.sub.11 is hydrogen; C1-30 alkyl; C.sub.2-30 alkenyl; C.sub.1-30 alkoxy; phenyl; C.sub.1 -20 alkylsulfonyl; or cholesteryl; and R.sub.4 may additionally be hydrogen; R.sub.5 is hydrogen; or R.sub.5 --R.sub.6 together is -CH.sub.2 -CH.sub.2 -CH.sub.2 ; R.sub.6 is hydrogn; C.sub.1-7 alkyl; hydroxymtehyl; mercaptomethyl; benzyl; or substituted benzyl; R.sub.7 and R.sub.8 may be the same or different and are each ndependently COOR or CONR' R", where R is hydrogen or C.sub.1-7 alkyl, and R' and R" are each independently hydrogen or C.sub.1-3 alkyl; when R.sub.2 is C.sub.1-10 alkyl, the stereochemistry at asymmetric p1 when R.sub.6 is not hydrogen, the stereochemistry at asymmetric center I can be either D or L; when R.sub.2 is C.sub.1-3 not hydrogen, the stereochemistry at center II is L; the stereochemistry at asymmetric center III is D; or pharmaceutically acceptable salts thereof; and an antiviral anti-AIDS drug selected from the group consisting of azidothymidine, ansamycin, ribavirin, deoxycytidine, HPA-23, AL-721, and foscarnet, ina physiologically acceptable medium in an amount effective to impart resistance against bacterial, fungal or viral infection. 2. The composition according to claim 1 wherein the compound is a preparation of 2-acetamido5, 6-di-O-acetyl-2-deoxy-3-O-(D-2-propionyl-L-alnayl-D-isoglutamine)-D-glucof uranose. 3. The composition according to claim 1 wherein the compound is a preparation of 2-acetamido-5-O-acetyl-2-deoxy-3-O-(D-2-propionyl-L-alanyl-D-isoglutamine) -6-0-stearoyl-D-glucofuranose. 4. The composition according to claim 1 wherein the compound is a preparation of 2-acetamido-5-O-acetyl-6-0-behenoyloxyisobutyryl-2-deosy-3-0(D-2-propionyl -L-alanyl-D-isoglutaimen)-D-glucofuranose. 5. A method for enhancing host resistance against opportunistic bacterial, fungal or viral infection in a human host immunocompromised by an AIDS-related virus comprising the step of administering to said host a composition containing a compound according to claim 1.

Details for Patent 4,866,036

Applicant	Tradename	Biologic Ingredient	Dosage Form	BLA	Approval Date	Patent No.	Expiredate
Hoffmann-la Roche Inc.	PEGASYS COPEGUS COMBINATION PACK	peginterferon alfa-2a and ribavirin		125083	June 04, 2004		2039-03-29
Schering Corporation A Subsidiary Of Merck & Co., Inc.	PEGINTRON/ REBETOL COMBO PACK	peginterferon alfa-2b and ribavirin		125196	June 13, 2008		2039-03-29